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Study of change of reactivation potency and also ability of penetration throught the blood-brain barrier of newly prepared (fluorinated) acetylcholinesterase reactivator
Jurczyk, Pavel ; Vopršalová, Marie (advisor) ; Žáčková, Pavla (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Ing. Pavel Jurczyk Supervisor: PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: Study of change of reactivation potency and also ability of penetration throught the blood-brain barrier of newly prepared (fluorinated) acetylcholinesterase reactivator The purpose of our experiment was to find that introduction of Fluor atom to the reactivator structure leads to higher potency of reactivation action or improved the ability to permeate into the brain. The higher concentration of effective oxime in the brain may leads to increasion of reactivation efficacy in the central nervous system. We compare therapeutical potency of this compound against commonly used not fluorinated oxim reactivators acetylcholinesterase by intoxication with tabun in vivo. Experiments were performed on male of laboratory Wistar rats. Atropin in the dose (21 mg/kg) in combination with reactivator 5 minutes before intoxication (1 LD50; 180 μg/kg) were applied intramuscularly. Thirty minutes after intoxications animals were killed in CO2 atmosphere and took up them blood, brain and diaphragm. The plasma was prepared by centrifugation of the blood at 3000 ot./min. by 10 0 C. The activity AChE and BuChE were...
Study of change of reactivation potency and also ability of penetration throught the blood-brain barrier of newly prepared (fluorinated) acetylcholinesterase reactivator
Jurczyk, Pavel ; Vopršalová, Marie (advisor) ; Žáčková, Pavla (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Ing. Pavel Jurczyk Supervisor: PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: Study of change of reactivation potency and also ability of penetration throught the blood-brain barrier of newly prepared (fluorinated) acetylcholinesterase reactivator The purpose of our experiment was to find that introduction of Fluor atom to the reactivator structure leads to higher potency of reactivation action or improved the ability to permeate into the brain. The higher concentration of effective oxime in the brain may leads to increasion of reactivation efficacy in the central nervous system. We compare therapeutical potency of this compound against commonly used not fluorinated oxim reactivators acetylcholinesterase by intoxication with tabun in vivo. Experiments were performed on male of laboratory Wistar rats. Atropin in the dose (21 mg/kg) in combination with reactivator 5 minutes before intoxication (1 LD50; 180 μg/kg) were applied intramuscularly. Thirty minutes after intoxications animals were killed in CO2 atmosphere and took up them blood, brain and diaphragm. The plasma was prepared by centrifugation of the blood at 3000 ot./min. by 10 0 C. The activity AChE and BuChE were...

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